Huperzine A water-soluble eye drops containing cyclodextrin or cyclodextrin derivatives, and preparation method and application of huperzine A water-soluble eye drops

A technology of huperzine A and cyclodextrin, which is applied in the field of medicine, can solve problems such as complicated preparation operations, difficulty in defining the prototype of huperzine A or its hydrochloride form, and high precision requirements

Pending Publication Date: 2021-06-29
HE EYE HOSPITAL SHENYANG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The operation is cumbersome and requires high precision. It is difficult to determine whether Huperzine A exists in the prototype or in the form of hydrochloride in the final aqueous solution.
Huperzine A is also dissolved in an oily medium, and then dispersed in water to form an emulsion to achieve its expected formulation specifications. During the preparation process, a large amount of surfactant is required to stabilize the emulsion system, and the preparation operation is more cumbersome.

Method used

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  • Huperzine A water-soluble eye drops containing cyclodextrin or cyclodextrin derivatives, and preparation method and application of huperzine A water-soluble eye drops
  • Huperzine A water-soluble eye drops containing cyclodextrin or cyclodextrin derivatives, and preparation method and application of huperzine A water-soluble eye drops
  • Huperzine A water-soluble eye drops containing cyclodextrin or cyclodextrin derivatives, and preparation method and application of huperzine A water-soluble eye drops

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0061] Example 1: Preparation of 0.001% Hydroxypropyl-β-cyclodextrin Huperzine A Water-Soluble Eye Drops

[0062] Weigh the materials according to the following proportions:

[0063]

[0064]

[0065] Add huperzine A and hydroxypropyl-β-cyclodextrin to part of the water for injection, stir at room temperature for 3 hours to dissolve them all, add other auxiliary materials in advance to prepare the aqueous solution for injection, and finally add water for injection to The whole amount is obtained by filtering through a 0.22 μm microporous membrane. The pH of the prepared eye drops is 7.33.

Embodiment 2

[0066] Example 2: Preparation of 0.005% Hydroxypropyl-β-cyclodextrin Huperzine A Water-Soluble Eye Drops

[0067] Weigh and take materials according to the following ratio:

[0068]

[0069] Add huperzine A and hydroxypropyl-β-cyclodextrin to part of the water for injection, stir at room temperature for 3 hours to dissolve them all, add other auxiliary materials in advance to prepare the aqueous solution for injection, and finally add water for injection to The whole amount is obtained by filtering through a 0.22 μm microporous membrane. The pH of the prepared eye drops is 7.52.

Embodiment 3

[0070] Embodiment 3: Preparation of 0.005% α-cyclodextrin huperzine A water-soluble eye drops

[0071] Weigh the materials according to the following proportions:

[0072]

[0073] Add huperzine A and α-cyclodextrin to part of the water for injection, stir at room temperature for 2.5 hours to dissolve them all, then add the aqueous solution for injection prepared in advance with other excipients, and finally add water for injection to the full amount, 0.22 μm Microporous membrane filtration, that is. The pH of the prepared eye drops is 7.75.

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Abstract

The invention provides huperzine A water-soluble eye drops containing cyclodextrin or cyclodextrin derivatives, a preparation method of the huperzine A water-soluble eye drops and application of the huperzine A water-soluble eye drops in preparation of a medicine for improving and treating presbyopia, and belongs to the technical field of medicines. The huperzine A water-soluble eye drops comprise huperzine A serving as an active component, a cyclodextrin or a cyclodextrin derivative serving as a solubilizer, a stabilizer, an osmotic pressure regulator and a bacteriostatic agent; and the molar ratio of the huperzine A serving as the active component to the cyclodextrin or the cyclodextrin derivative serving as the solubilizer is 1:(4-10). The preparation method disclosed by the invention comprises the following steps of: adding the cyclodextrin or the cyclodextrin derivative and the huperzine A into the water for injection, performing stirring at room temperature to completely dissolve the cyclodextrin or the cyclodextrin derivative and the huperzine A, adding an aqueous solution for injection prepared by other auxiliary materials in advance, supplementing the water for injection to full dose, and filtering by a microporous filter membrane to obtain the huperzine A water-soluble eye drops. The huperzine A water-soluble eye drops disclosed by the invention have small irritation to eyes and good stability, and can effectively shrink pupils and improve and treat presbyopia caused by aging.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a water-soluble eye drop of huperzine A containing cyclodextrin or cyclodextrin derivatives, a preparation method thereof, and an application in preparation of medicines for improving and treating presbyopia. Background technique [0002] Presbyopia is the most common visual problem when people enter middle-aged and old age, and it is one of the signs that the body begins to age. With age, the lens of the eyeball gradually hardens and thickens, and the adjustment ability of the eye muscles also decreases, resulting in a decrease in zooming ability, and images from close distances cannot be focused on the retina for clear imaging, thus making it difficult to see nearby objects clearly . The occurrence and development of presbyopia are directly related to age, and most of them appear after the age of 45. In recent years, some ophthalmologists also said that the exces...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K31/4748A61K47/40A61P27/10
CPCA61K9/08A61K9/0048A61K31/4748A61K47/40A61P27/10
Inventor 何伟何向东张东蕾王敏楠安元龙杜国新
Owner HE EYE HOSPITAL SHENYANG
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